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BAY-784 | BAY-784 : Antagonist of GNRHR
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
GNRHR
  • IC50:27 nM
  • IC50:21 nM
Antagonist
up to 10 µM
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selectivity within target family: Selectivity against a broad range of GPCR‘s. Clean GPCR scan excep ...

Potency
Cellular
In Vitro

GNRHR

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.0c01076

In Vivo Validations

Rat
Dose: 0.5 mg/kg IV, 2.0, 10 and 30 mg/kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 13-17 h
Systemic clearance: 0.54 L/h/kg
Area Under the Curve:: 0.8-1.4 kg·h/L
Bioavailability: 48-87%
Volume of Distribution at Steady-State: 10 L/Kg
Target engagement assay: has been used in efficacy models at doses of 10 and 30 mg/kg po in the rat

DOI Reference: 10.1021/acs.jmedchem.0c01076

Dog
Dose: 0.5 mg/kg IV, 2.0 mg/kg PO
Route of delivery: Intravenous. Oral
Plasma half life: 18 h
Systemic clearance: 0.66 L/h/kg
Area Under the Curve:: 1.4 kg·h/L
Bioavailability: 69%
Volume of Distribution at Steady-State: 6.3 L/Kg

DOI Reference: 10.1021/acs.jmedchem.0c01076

Monkey (Cynomolgus)
Dose: 0.5 mg/kg IV, 2.0 and 20 mg/kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 7 h
Systemic clearance: 1.0 L/h/kg
Area Under the Curve:: 0.2-0.5 kg·h/L
Bioavailability: 16-40%
Volume of Distribution at Steady-State: 3.6 L/Kg
Target engagement assay: Has been used in monkey (ORX) efficacy models at doses of 20 mg/kg po in cynymologous monkey.

DOI Reference: 10.1021/acs.jmedchem.0c01076

Negative Control Compounds

BAY-786
Notes: The control compound BAY-786 has at least 114-fold lower in vitro potency (IC50 = 2.4 μM). Clean GPCR scan except for weak activity on TMEM97 (Ki = 2001.24 nM)

Chemical Information

Molecular Formula C29H26ClF4N3O5S2
SMILEs O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1
InChI InChI=1S/C29H26ClF4N3O5S2/c30-23-14-19(29(32,33)34)15-35-24(23)16-36-27(38)18-3-8-25-22(13-18)28(9-11-43(39,40)12-10-28)26(17-1-2-17)37(25)44(41,42)21-6-4-20(31)5-7-21/h3-8,13-15,17,26H,1-2,9-12,16H2,(H,36,38)/t26-/m0/s1
Molecular weight 671.09 Da
AlogP 5.2568000000000055
HBond acceptors 8
HBond donors 1
Atoms 70

Vendors

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Expert Reviews

by SERP
(on 5 Feb 2022 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 18 Feb 2022 )
Cellular Use Rating
In Model Organisms
Probe BAY-784 is an effective "partial antagonist" of GNRHR at two digit nanomolar, it can reduce the LH level ~up to 50% from base level in various testing model (cell, animal, human). For off-target...
by SERP+
(on 14 Oct 2025 )
Cellular Use Rating
In Model Organisms
This is a well validated compound. It would have been useful to see Cmax. The unbound fraction is low for this clinical candidate 5a/BAY-1214784 (1.4%).
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria